DIETARY HYPOCHOLESTEROLAEMIC COMPOSITIONS COMPRISING SOYA PROTEINS AND SITOSTEROLS

Abstract: Description of dietary compositions for use as nutritional integrators containing a mixture of soya proteins and sitosterols.

Description: DIETARY HYPOCHOLESTEROLAEMIC COMPOSITIONS COMPRISING SOYA PROTEINS AND SITOSTEROLS This invention refers to a composition for oral administration consisting of an association of substances of natural origin which exert a hypocholesterolaemic action. The types of vascular damage that can be caused by a hypercholesterolaemic condition are numerous and a balanced diet plays a role of primary importance in the prevention of such alterations (1) (2). The populations more exposed to this type of pathology are the richer ones whose normal everyday diet, apart from being unbalanced, often exceeds daily requirements. Hypercholesterolaemia can be treated either pharmacologically or by undertaking preventive action in terms of modifiying or integrating the usual nutritional intake. The invention regards a preparation for oral administration that associates Soya proteins with sitosterols, as integrators of the habitual diet. The influence of Soya proteins on nutrition is known both in normal cholesterol level and in hypercholesterolaemic conditions (3). Sitosterols, beta-sitosterols in particular, are substances that are used extensively in hypocholesterolaemic treatments (4) (5). Their chemical structure, similar to cholesterol, differs because of an ethyl group bound to the carbon in position 24, provides these substances with an absorption behaviour which is very different from that of cholesterol. These substances, contrary to the cholesterol contained in food, are not absorbed and interfere with the absorption of the cholesterol taken in. The limited food absorption causes a consequent and significant hypocholesterolaemic effect (6). Hypocholesterolaemic treatments with Soya proteins or with sitosterols described in literature refer to high daily quantities. Certain studies describe diets of 10-15 g/day with isolated Soya proteins or 12 g/day for sitosterols. The invention regards the synergistic activity of the two hypocholesterolaemic substances which, if associated, can reduce the daily dose to be used in a hypocholesterolaemic diet by ten times. The synergistic effect claimed by the invention enables administration of low quantities of hypocholesterolaemic integrators for long periods with consequent decrease of sitosterolemic risk. The daily dose of the hypocholesterolaemic association can therefore be 1-2 g/day of the combination. The dietary compositions of the invention may contain from 50 to 2000 mg of Soya proteins. The quantity of sitosterols per unit can vary from 10 to 1000 mg. The ponderal ratio between Soya proteins and sitosterols is not crucial and will generally be between 1:1 and 10:1. The compositions which are the subject of the invention may also contain active principles or integrators with coadjuvant, complementary or useful activity. Examples of these elements which can be usefully employed for the purpose are: mineral salts vitamins digestive enzymes soluble fibres insoluble fibres amino acids phospholipids The compositions which are the subject of the invention are prepared using traditional techniques and excipients. These compositions are prepared by mixing Soya proteins and sitosterols with excipients that are physiologically suitable and with pleasant appearance, colour and flavour. Among the excipients available for alimentary use are diluting agents, sweeteners, binding agents, flavouring agents, lubricants, anti- aggregating agents, natural and synthetic colouring agents, solubilizers, surfactants and preservatives. Examples of diluting substances are: microcrystalline cellulose, lactose, glycine, rice starch, saccharose, fructose, sorbitol; examples of binding agents are: starch water, pvp, methylcellulose; examples of flavouring agents are: citric acid, tartaric acid, sodium chloride, sodium glutamate, menthol; examples of lubricants are: PEG, magnesium stearate, stearic acid, talc. The examples of dietary compositions include: chewable, effervescent, swallowable and coated tablets; film coated pills, capsules, soft gelatine capsules, syrup, fruit beverages, granule sachets, fruit gelatines, sweets. The following are hypocholesterolaemic dietary formulations: Coated tablets Tablets Soya proteins 300 mg sitosterols 200 mg maize starch 30 mg pvp 20 mg lactose 50 mg talc 10 mg magnesium stearate 5 mg Granules for extemporaneous suspension Soya proteins 800 mg sitosterols 200 mg saccharose 2000 mg sodium saccharinate 20 mg apple flavouring 50 mg Capsules Soya proteins 100 mg sitosterols 100 mg magnesium stearate 10 mg Silica precipitate 5 mg SHELL gelatin 100 mg Chewable tablets Soya proteins 300 mg sitosterols 200 mg mannitol 500 mg pvp 20 mg sorbitol 100 mg aspartame 3 mg magnesium stearate 5 mg The dietary preparations based on Soya proteins/sitosterols can be associated with substances such as food fibres (soluble or insoluble) to produce dietary hypocholesterolaemic-bulking agents. The following is an example of a formulation: HYPOCHOLESTEROLAEMIC - BULKING AGENT Granules for extemporaneous suspension Soya proteins 800 mg sitosterols 200 mg guar gum 2000 mg saccharose 1000 mg sodium saccharinate 20 mg Orange flavouring 50 mg The hypocholesterolaemic association combined with enzymes of vegetable origin such as bromelain gives hypocholesterolaemic-digestive products. The following is an example of a formulation: HYPOCHOLESTEROLAEMIC-DIGESTIVE PRODUCT Chewable tablets Soya proteins 300 mg sitosterols 200 mg bromelain 10 mg mannitol 500 mg pvp 20 mg sorbitol 100 mg aspartame 3 mg magnesium stearate 5 mg

Claims: CLAIMS 1. Hypocholesterolaemic compositions containing Soya proteins associated synergistically with sitosterols. 2. Compositions according to claim 1 , containing from 50 mg to 2000 mg of Soya proteins and from 10 mg to 1000 mg of sitosterols per unit. 3. Compositions according to any of the previous claims containing other active principles or integrators with a coadjuvant, complementary or useful activity. 4. Compositions according to claims 2 or 3, containing also at least one substance chosen from the group comprising: mineral salts, vitamins, digestive enzymes, soluble fibres, insoluble fibres, amino acids and phospholipids. 5. Compositions according to any of the previous claims in the form of chewable, effervescent, swallowable and coated tablets, capsules, soft gelatine capsules, syrup, fruit beverages, granule sachets, fruit gelatines, sweets.

Inventors: FESTOE NORBERTO, FESTOE, NORBERTO
Applicants: FESTOE NORBERTO, INPHARMA SA, FESTOE, NORBERTO, INPHARMA S.A.
Application year: 1994
Main classification: A61K38
IPC codes: A23G3, A23G4, A23L1, A23L2, A61K31, A61K36, A61K38, A61P3